Fully Automated Radiosynthesis of 2-[18F]Fludarabine for PET Imaging of Low-Grade Lymphoma

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• 作者：Stéphane Guillouet (1) (2) (3)
  Delphine Patin (1) (2) (3) (4)
  Olivier Tirel (1) (2) (3)
  Jér?me Delamare (1) (2) (3)
  Fabienne Gourand (1) (2) (3)
  Jean Bernard Deloye (4)
  Michel Leporrier (1) (2) (3)
  Louisa Barré (1) (2) (3)
  
• 关键词：F ; 18 labeling ; 2 ; [18F]Fludarabine ; Automated radiosynthesis ; PET ; Nucleoside ; Lymphoma
• 刊名：Molecular Imaging and Biology
• 出版年：2014
• 出版时间：February 2014
• 年：2014
• 卷：16
• 期：1
• 页码：28-35
• 全文大小：512 KB
• 作者单位：Stéphane Guillouet (1) (2) (3)
  Delphine Patin (1) (2) (3) (4)
  Olivier Tirel (1) (2) (3)
  Jér?me Delamare (1) (2) (3)
  Fabienne Gourand (1) (2) (3)
  Jean Bernard Deloye (4)
  Michel Leporrier (1) (2) (3)
  Louisa Barré (1) (2) (3)
  
  1. CEA, I2BM, LDM-TEP, UMR 6301 ISTCT, GIP Cyceron, 14074, Caen, France
  2. CNRS, UMR 6301 ISTCT, LDM-TEP, GIP Cyceron, Bd Henri Becquerel, BP 5229, 14074, Caen Cedex, France
  3. Université de Caen Basse-Normandie, UMR 6301 ISTCT, LDM-TEP, GIP Cyceron, 14074, Caen, France
  4. Laboratoires CYCLOPHARMA, Biop?le Clermont–Limagne, 63360, Saint Beauzire, France
  
• ISSN：1860-2002

文摘

Purpose An efficient and fully automated radiosynthesis of 2-[18F]fluoro-9-β-d-arabinofuranosyl-adenine (2-[18F]fludarabine, [18F]-5) based on a GE TRACERlab?FX-FN module has been developed. Procedures A 2-nitro purine derivative 3 was developed as precursor for labeling with fluorine-18. The radiosynthesis of [18F]-5 was performed in two steps in a single reactor with an intermediary purification on Sep-Pak? silica which involved the addition of a three-way valve on the original module. After hydrolysis, [18F]-5 was purified by semi-preparative high-pressure liquid chromatography (HPLC) and a quality control was established. Results The labeling precursor 3 was obtained in 45?% overall yield. Nucleophilic substitution with K18F/K2.2.2 afforded protected 2-[18F]fludarabine ([18F]-4) in 73?±-?% , radiochemical yield (decay corrected to the end of bombardment (EOB)) and based on the initial [18F]F?/sup> activity. An aqueous ammonia/methanol solution was used for the deprotection reaction and gave the desired [18F]-5 in 67?±-?% yield after 20?min at 70?°C based on HPLC profile. Conclusions The process afforded pure 2-[18F]fludarabine in 48?±-?% yield (decay corrected to the EOB) in 85?min, with a specific activity of 310?±-2?GBq/μmol at the end of synthesis (EOS) and a radiochemical purity up to 99?%.